Abstract
The synthesis of novel tetrazole/sulfonamide derivatives based on octahydroacridine, xanthene and chromene scaffold by using microwave (MW) assisted techniques is reported in this study. These synthesized hybrid compounds were assayed for the inhibition of carbonic anhydrase (CA, EC 4.2.1.1). The inhibitory activities were determined against three cytosolic human isoforms (hCA I, II and VII) and one membrane-associated (hCA IV) isoform. Some of the newly synthesized sulfonamides showed micromolar to nanomolar inhibitory activity against these enzymes.
Keywords:
Carbonic anhydrase; Chromene; Enzyme inhibition; Octahydroacridine; Sulfonamide; Tetrazole.
Copyright © 2016 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Acridines / chemistry
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Acridines / pharmacology
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Benzopyrans / chemistry
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Benzopyrans / pharmacology
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Carbonic Anhydrase Inhibitors / chemical synthesis
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Carbonic Anhydrase Inhibitors / chemistry
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Carbonic Anhydrase Inhibitors / pharmacology*
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Carbonic Anhydrases / metabolism*
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Dose-Response Relationship, Drug
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Humans
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Isoenzymes / antagonists & inhibitors
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Isoenzymes / metabolism
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Microwaves*
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Molecular Structure
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Structure-Activity Relationship
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Sulfonamides / chemical synthesis
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Sulfonamides / chemistry
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Sulfonamides / pharmacology*
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Tetrazoles / chemical synthesis
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Tetrazoles / chemistry
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Tetrazoles / pharmacology*
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Xanthenes / chemistry
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Xanthenes / pharmacology
Substances
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1,2,3,4,5,6,7,8-octahydroacridine
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Acridines
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Benzopyrans
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Carbonic Anhydrase Inhibitors
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Isoenzymes
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Sulfonamides
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Tetrazoles
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Xanthenes
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Carbonic Anhydrases